1t54
From Proteopedia
(New page: 200px<br /><applet load="1t54" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t54" /> '''Antibiotic Activity and Structural Analysis ...) |
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'''Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs'''<br /> | '''Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs'''<br /> | ||
==Overview== | ==Overview== | ||
| - | IsCT is a non-cell-selective antimicrobial peptide isolated from the | + | IsCT is a non-cell-selective antimicrobial peptide isolated from the scorpion Opisthacanthus madagascariensis that has potent cytolytic activity against both mammalian and bacterial cells. To investigate the structure-activity relationships of IsCT and to design novel peptide antibiotics with bacterial cell selectivity, we synthesized several analogs of IsCT and determined their three-dimensional structures in solution by 2D-NMR spectroscopy. IsCT has a linear alpha-helical structure from Gly3 to Phe13, and [K7]-IsCT has a linear alpha-helical structure from Leu2 to Phe13. [K7, P8, K11]-IsCT, which has a bend in its middle region, exhibited the highest antibacterial activity without hemolytic activity, suggesting that its proline-induced bend is an important determinant of this selectivity. Tryptophan fluorescence showed that the high selectivity of [K7, P8, K11]-IsCT toward bacterial cells is closely correlated with its highly selective interaction with negatively charged phospholipids. Its potent activity against antibiotic-resistant bacteria suggests that [K7, P8, K11]-IsCT may serve as a promising lead candidate in the development of new peptide antibiotics. |
==About this Structure== | ==About this Structure== | ||
| - | 1T54 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Opisthacanthus_madagascariensis Opisthacanthus madagascariensis] with NH2 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 1T54 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Opisthacanthus_madagascariensis Opisthacanthus madagascariensis] with <scene name='pdbligand=NH2:'>NH2</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T54 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Opisthacanthus madagascariensis]] | [[Category: Opisthacanthus madagascariensis]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
| - | [[Category: Hahm, K | + | [[Category: Hahm, K S.]] |
[[Category: Kim, K.]] | [[Category: Kim, K.]] | ||
[[Category: Kim, Y.]] | [[Category: Kim, Y.]] | ||
[[Category: Lee, K.]] | [[Category: Lee, K.]] | ||
| - | [[Category: Lim, S | + | [[Category: Lim, S S.]] |
| - | [[Category: Shin, S | + | [[Category: Shin, S Y.]] |
[[Category: NH2]] | [[Category: NH2]] | ||
[[Category: coil-helix]] | [[Category: coil-helix]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:09:58 2008'' |
Revision as of 13:09, 21 February 2008
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Antibiotic Activity and Structural Analysis of a Scorpion-derived Antimicrobial peptide IsCT and Its Analogs
Overview
IsCT is a non-cell-selective antimicrobial peptide isolated from the scorpion Opisthacanthus madagascariensis that has potent cytolytic activity against both mammalian and bacterial cells. To investigate the structure-activity relationships of IsCT and to design novel peptide antibiotics with bacterial cell selectivity, we synthesized several analogs of IsCT and determined their three-dimensional structures in solution by 2D-NMR spectroscopy. IsCT has a linear alpha-helical structure from Gly3 to Phe13, and [K7]-IsCT has a linear alpha-helical structure from Leu2 to Phe13. [K7, P8, K11]-IsCT, which has a bend in its middle region, exhibited the highest antibacterial activity without hemolytic activity, suggesting that its proline-induced bend is an important determinant of this selectivity. Tryptophan fluorescence showed that the high selectivity of [K7, P8, K11]-IsCT toward bacterial cells is closely correlated with its highly selective interaction with negatively charged phospholipids. Its potent activity against antibiotic-resistant bacteria suggests that [K7, P8, K11]-IsCT may serve as a promising lead candidate in the development of new peptide antibiotics.
About this Structure
1T54 is a Single protein structure of sequence from Opisthacanthus madagascariensis with as ligand. Full crystallographic information is available from OCA.
Reference
Antibiotic activity and structural analysis of the scorpion-derived antimicrobial peptide IsCT and its analogs., Lee K, Shin SY, Kim K, Lim SS, Hahm KS, Kim Y, Biochem Biophys Res Commun. 2004 Oct 15;323(2):712-9. PMID:15369808
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